BPI-2009

BPI-2009 Uses, Dosage, Side Effects, Food Interaction and all others data.

BPI-2009 is a potent and specific epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI)BPI-2009 was approved in China by the SFDA in June, 2011 and in January 2014, Beta Pharma, Inc. was given a “May Proceed” from the US FDA to conduct a Phase I study for the evaluation of icotinib as a treatment of EGFR+ Non-Small Cell Lung Cancer (NSCLC).

In vitro: BPI-2009 inhibits EGFR activity in a dose-dependent manner, with an IC50 value of 5 nM and complete inhibition at 62.5 nM. BPI-2009 selectively solely inhibits the EGFR members including the wild type and mutants with inhibition efficacies of 61-99%. BPI-2009 blocks EGFR-mediated intracellular tyrosine phosphorylation in human epidermoid carcinoma A431 cells in a dose-dependent manner. Meanwhile, in the proliferation assay performed on A431, BGC-823, A549, H460, HCT8, KB and Bel-7402 cell lines, it was found that the relative sensitivity of cell lines to BPI-2009 is A431 > BGC-823 > A549 > H460 > KB > HCT8 and Bel-7402. BPI-2009 exhibits a broad spectrum of antitumor activity and it is especially effective against tumors expressing higher levels of EGFR.In vivo: In vivo studies demonstrated that BPI-2009 exhibited potent dose-dependent antitumor effects in nude mice carrying a variety of human tumor-derived xenografts. The drug was well tolerated at doses up to 120 mg/kg/day in mice without mortality or significant body weight loss during the treatment. A head to head randomized, double blind phase III trial using Gefitinib as an active control for patients with advanced non-small cell lung cancer (NSCLC) was finished recently (Trial registration ID: NCT01040780).

BPI-2009
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Trade Name	BPI-2009
Generic	Icotinib
Icotinib Other Names	BPI-2009
Type
Formula	C₂₂H₂₁N₃O₄
Weight	Average: 391.427 Monoisotopic: 391.153206168
Protein binding	Icotinib binds to Sudlow's site I in subdomain IIA of Human Serum Albumin (HSA) molecule, resulting in the formation of icotinib-HSA complexes.
Groups	Experimental, Investigational
Therapeutic Class
Manufacturer
Available Country
Last Updated:	September 19, 2023 at 7:00 am

Uses

BPI-2009 hydrochloride is a novel epidermal growth factor receptor (EGFR)–tyrosine kinase inhibitor, exhibits encouraging efficacy and tolerability in patients with advanced non-small-cell lung cancer (NSCLC) who failed previous chemotherapy.

How BPI-2009 works

BPI-2009 is a highly selective, first generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) which binds reversibly to the ATP binding site of the EGFR protein, preventing completion of the signal transduction cascade. EGFR is an oncogenic receptor and patients with activating somatic mutations, such as an exon 19 deletion or exon 21 L858R mutation, within the tyrosine kinase domain display unchecked cell proliferation.